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AR104326A1 - 5-SUBSTITUTED NUCLEOSID COMPOUNDS - Google Patents

5-SUBSTITUTED NUCLEOSID COMPOUNDS

Info

Publication number
AR104326A1
AR104326A1 ARP160101081A ARP160101081A AR104326A1 AR 104326 A1 AR104326 A1 AR 104326A1 AR P160101081 A ARP160101081 A AR P160101081A AR P160101081 A ARP160101081 A AR P160101081A AR 104326 A1 AR104326 A1 AR 104326A1
Authority
AR
Argentina
Prior art keywords
cancer
compounds
hydrogen
fluoro
chlorine
Prior art date
Application number
ARP160101081A
Other languages
Spanish (es)
Original Assignee
Lilly Co Eli
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR104326A1 publication Critical patent/AR104326A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14Pyrrolo-pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente solicitud se refiere a compuestos nucleósidos 5-sustituidos, composiciones farmacéuticas que comprenden los compuestos, y métodos de utilización de los compuestos para el tratamiento del cáncer, en particular los glioblastomas, melanoma, sarcomas, cáncer gástrico, cáncer de páncreas, colangiocarcinoma, cáncer de vejiga, cáncer de mama, cáncer de pulmón de células no pequeñas, leucemias, incluyendo leucemia mieloide aguda y los linfomas. Reivindicación 1: Un compuesto de la fórmula (1) donde: R¹ᵃ es hidrógeno, C₁₋₂ alquilo, C₃₋₆ cicloalcoxi, trifluorometil, ciano, cloro, o fluoro; R¹ᵇ es hidrógeno, cloro, o fluoro; R² es hidrógeno o C₁₋₃ alquilo; y R³ es hidrógeno, metil o amino; o una sal de la misma aceptable para uso farmacéutico.The present application relates to 5-substituted nucleoside compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer, in particular glioblastomas, melanoma, sarcomas, gastric cancer, pancreatic cancer, cholangiocarcinoma, Bladder cancer, breast cancer, non-small cell lung cancer, leukemia, including acute myeloid leukemia and lymphomas. Claim 1: A compound of the formula (1) wherein: R¹ᵃ is hydrogen, C₁₋₂ alkyl, C₃₋₆ cycloalkoxy, trifluoromethyl, cyano, chlorine, or fluoro; R¹ᵇ is hydrogen, chlorine, or fluoro; R² is hydrogen or C₁₋₃ alkyl; and R³ is hydrogen, methyl or amino; or a salt thereof acceptable for pharmaceutical use.

ARP160101081A 2015-05-04 2016-04-20 5-SUBSTITUTED NUCLEOSID COMPOUNDS AR104326A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP15382225 2015-05-04

Publications (1)

Publication Number Publication Date
AR104326A1 true AR104326A1 (en) 2017-07-12

Family

ID=53177322

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160101081A AR104326A1 (en) 2015-05-04 2016-04-20 5-SUBSTITUTED NUCLEOSID COMPOUNDS

Country Status (25)

Country Link
US (1) US9840532B2 (en)
EP (1) EP3292128A1 (en)
JP (2) JP6181889B1 (en)
KR (1) KR20170132871A (en)
CN (1) CN107580602A (en)
AR (1) AR104326A1 (en)
AU (1) AU2016258485A1 (en)
BR (1) BR112017020336A2 (en)
CA (1) CA2981097A1 (en)
CL (1) CL2017002637A1 (en)
CO (1) CO2017010727A2 (en)
CR (1) CR20170443A (en)
DO (1) DOP2017000255A (en)
EA (1) EA201792169A1 (en)
EC (1) ECSP17072987A (en)
HK (1) HK1244007A1 (en)
IL (1) IL254409A0 (en)
MA (1) MA42036A (en)
MX (1) MX2017014001A (en)
PE (1) PE20180231A1 (en)
PH (1) PH12017502002A1 (en)
SG (1) SG11201708345XA (en)
TN (1) TN2017000459A1 (en)
TW (1) TWI615400B (en)
WO (1) WO2016178870A1 (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3262057B1 (en) * 2015-02-24 2020-04-15 Pfizer Inc Substituted nucleoside derivatives useful as anticancer agents
JP7043080B2 (en) * 2017-01-27 2022-03-29 国立大学法人 宮崎大学 Efficacy judgment kit for cancer and efficacy judgment method for cancer
WO2018152501A1 (en) 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2018152548A1 (en) 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2018160855A1 (en) 2017-03-01 2018-09-07 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
EP3665179B1 (en) 2017-08-09 2021-06-09 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
JP7328218B2 (en) 2017-10-26 2023-08-16 プレリュード セラピューティクス,インコーポレイティド Selective inhibitor of protein arginine methyltransferase 5 (PRMT5)
CU24621B1 (en) 2017-12-13 2022-09-08 Lupin Ltd SUBSTITUTED BICYCLIC HETEROCYCLIC COMPONENTS AS PRMT5 INHIBITORS
US10711007B2 (en) 2018-03-14 2020-07-14 Prelude Therapeutics Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
DK3765461T3 (en) 2018-03-14 2023-11-20 Prelude Therapeutics Inc SELECTIVE PROTEIN ARGININE METHYL TRANSFERASE 5 (PRMT5) INHIBITORS
JP7337539B2 (en) * 2018-06-21 2023-09-04 メディヴィル・アクチエボラーグ Base-Modified Cytidine Nucleotides for Leukemia Therapy
WO2020033285A1 (en) * 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US20220160713A1 (en) * 2019-02-13 2022-05-26 Prelude Therapeutics, Incorporated Selective inhibitor of protein arginine methyltransferase 5 (prmt5)
WO2020206299A1 (en) 2019-04-05 2020-10-08 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5
CR20220010A (en) 2019-06-10 2022-05-13 Lupin Ltd PRMT5 INHIBITORS
US12414953B2 (en) 2019-09-18 2025-09-16 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
MX2022004917A (en) 2019-10-22 2022-08-04 Lupin Ltd Pharmaceutical combination of prmt5 inhibitors.
US20230066014A1 (en) 2019-12-03 2023-03-02 Lupin Limited Substituted nucleoside analogs as prmt5 inhibitors
GB202117230D0 (en) 2021-11-29 2022-01-12 Argonaut Therapeutics Ltd Peptide vaccine
GB202203588D0 (en) 2022-03-15 2022-04-27 Argonaut Therapeutics Ltd Cancer diagnostic
CN116211869B (en) * 2022-12-07 2023-08-01 浙江省肿瘤医院 Drug mixture containing DNA damage repair inhibitor, mixing method and use
WO2026008533A1 (en) 2024-07-01 2026-01-08 Janssen Pharmaceutica Nv Prmt5 inhibitors for treating adenomas

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK1772002A3 (en) 1999-08-27 2002-10-08 Icn Pharmaceuticals Nucleoside analog, method of change of cytokine secreting from a cell and method for inhibiting the growth of hyperproliferative cells
NZ544187A (en) * 2005-12-15 2008-07-31 Ind Res Ltd Deazapurine analogs of 1'-aza-l-nucleosides
WO2011079236A1 (en) 2009-12-22 2011-06-30 The Ohio State University Research Foundation Compositions and methods for cancer detection and treatment
US9416154B2 (en) * 2011-07-13 2016-08-16 Merck Sharp & Dohme Corp. 5′-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
US8906900B2 (en) 2012-12-21 2014-12-09 Epizyme, Inc. PRMT5 inhibitors and uses thereof
WO2014100716A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US9745291B2 (en) 2012-12-21 2017-08-29 Epizyme, Inc. PRMT5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
HRP20182037T1 (en) 2012-12-21 2019-02-08 Epizyme, Inc. PRMT5 INHIBITORS AND THEIR USE
US20150344457A1 (en) 2012-12-21 2015-12-03 Epizyme, Inc. Methods of inhibiting prmt5
WO2014100734A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP3262057B1 (en) * 2015-02-24 2020-04-15 Pfizer Inc Substituted nucleoside derivatives useful as anticancer agents

Also Published As

Publication number Publication date
ECSP17072987A (en) 2018-02-28
SG11201708345XA (en) 2017-11-29
TW201712022A (en) 2017-04-01
DOP2017000255A (en) 2018-01-15
PE20180231A1 (en) 2018-01-31
MA42036A (en) 2018-03-14
US9840532B2 (en) 2017-12-12
KR20170132871A (en) 2017-12-04
BR112017020336A2 (en) 2019-05-14
TWI615400B (en) 2018-02-21
MX2017014001A (en) 2018-03-16
JP2017125029A (en) 2017-07-20
IL254409A0 (en) 2017-11-30
TN2017000459A1 (en) 2019-04-12
JP2017525667A (en) 2017-09-07
PH12017502002A1 (en) 2018-03-26
JP6181889B1 (en) 2017-08-16
AU2016258485A1 (en) 2017-10-12
CO2017010727A2 (en) 2018-01-31
US20160326208A1 (en) 2016-11-10
CA2981097A1 (en) 2016-11-10
EP3292128A1 (en) 2018-03-14
WO2016178870A1 (en) 2016-11-10
CR20170443A (en) 2017-11-07
HK1244007A1 (en) 2018-07-27
EA201792169A1 (en) 2018-03-30
CN107580602A (en) 2018-01-12
CL2017002637A1 (en) 2018-04-20

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